A cell-permeable salicylic acid compound that acts as a highly potent, active-site directed and substrate competitive AKR1C1 inhibitor (Ki=4nM) with moderate to excellent selectivity over AKR1C2, AKR1C3 and AKR1C4 (Ki=0.087, 4.2 and 18.2uM, respectively). Shown to inhibit the metabolism of progesterone by AKR1C1 (IC50=460nM in AKR1C1 overexpressing BAECs).
Synonyms:Aldo-Keto Reductase family 1 member C1 Inhibitor, 5-PBSA, 3-Bromo-5-phenylsalicylic acid, 20α-Hydroxysteroid Dehydrogenase Inhibitor, 5-PBSA
Molecular Formula:C₁₃H₉BrO₃
Solubility:DMSO
NMR:Conforms
LC-MS:Conforms
Purity:≥94% (HPLC)
Appearance:White solid.
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months after receipt at -20°C. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
